Background: There is a need for new small molecule pre-mRNA splicing inhibitors as biotools.Results: High throughput screening resulted in the identification of small molecule splicing inhibitors that are active in vitro and in cells.Conclusion: New small molecules for studying pre-mRNA splicing in vitro and in cells are identified.Significance: Small drug-like molecules are identified that modulate splicing in vitro and in cells.

We have developed a catalytic method for the hydroalkylation of allenes using alkyl triflates as electrophiles and silane as a hydride source. The reaction has an excellent substrate scope and is compatible with a wide range of functional groups, including esters, aryl halides, aryl boronic esters, sulfonamides, alkyl tosylates, and alkyl bromides. We found evidence for a reaction mechanism that involves unusual dinuclear copper ally complexes as catalytic intermediates. The unusual structure of these complexes provides a rationale for their unexpected reactivity.

The synthesis and directed dihydroxylation of a range of cyclic alkenes was investigated. Both homoallylic alcohols and homoallylic trihaloacetamides were found to be efficient directing groups, giving rise to good to excellent levels of remote asymmetric induction with OsO4-TMEDA. Interestingly, in all cases examined, trifluoroacetamides were found to be superior to trichloroacetamides as directing groups and an argument is presented which rationalises this observation.

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We have developed ac atalytic method for the hydroalkylation of allenes using alkylt riflates as electrophiles and silane as ah ydride source.T he reaction has an excellent substrate scope and is compatible with aw ide range of functional groups,i ncluding esters,a ryl halides,a ryl boronic esters,s ulfonamides,a lkylt osylates,a nd alkylb romides.W e found evidence for areaction mechanism that involves unusual dinuclear copper ally complexes as catalytic intermediates.The unusual structure of these complexes provides ar ationale for their unexpected reactivity. Scheme 1. Copper-catalyzed hydroalkylation of allenes.

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Hydroxylation Hydroxylation O 0216Scope of the Directed Dihydroxylation: Application to Cyclic Homoallylic Alcohols and Trihaloacetamides. -A range of cyclic homoallylic alcohols and amides are prepared in order to test their ability to direct dihydroxylation by hydrogen bonding to the OsO4-TMEDA reagent. Both alcohols and amides are found to be efficient directing groups, giving rise to good to excellent levels of remote asymmetric induction with this reagent, except for compounds with steric hindrance. In every case, dihydroxylation under standard oxidizing condition is also performed for comparison. Interestingly, trifluoroacetamides are found to be superior to trichloroacetamides as directing groups. -(DONOHOE*, T. J.; MITCHELL, L.; WARING, M. J.; HELLIWELL, M.; BELL, A.; NEWCOMBE, N.